EP4302761A3 - Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making - Google Patents

Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making Download PDF

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Publication number
EP4302761A3
EP4302761A3 EP23195076.7A EP23195076A EP4302761A3 EP 4302761 A3 EP4302761 A3 EP 4302761A3 EP 23195076 A EP23195076 A EP 23195076A EP 4302761 A3 EP4302761 A3 EP 4302761A3
Authority
EP
European Patent Office
Prior art keywords
methods
crystalline forms
making
ethan
triazin
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP23195076.7A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP4302761A2 (en
Inventor
Brian HEINRICH
Gordon Wilkie
Joshua D. WAETZIG
Lauren MACEACHERN
Brenton MAR
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Blueprint Medicines Corp
Original Assignee
Blueprint Medicines Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=70476546&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EP4302761(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Blueprint Medicines Corp filed Critical Blueprint Medicines Corp
Publication of EP4302761A2 publication Critical patent/EP4302761A2/en
Publication of EP4302761A3 publication Critical patent/EP4302761A3/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EP23195076.7A 2019-04-12 2020-04-10 Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making Pending EP4302761A3 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962833527P 2019-04-12 2019-04-12
US201962844575P 2019-05-07 2019-05-07
US202062990269P 2020-03-16 2020-03-16
PCT/US2020/027724 WO2020210669A1 (en) 2019-04-12 2020-04-10 Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making
EP20722936.0A EP3856341B1 (en) 2019-04-12 2020-04-10 Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making

Related Parent Applications (1)

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EP20722936.0A Division EP3856341B1 (en) 2019-04-12 2020-04-10 Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making

Publications (2)

Publication Number Publication Date
EP4302761A2 EP4302761A2 (en) 2024-01-10
EP4302761A3 true EP4302761A3 (en) 2024-03-27

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EP23195076.7A Pending EP4302761A3 (en) 2019-04-12 2020-04-10 Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making
EP20722936.0A Active EP3856341B1 (en) 2019-04-12 2020-04-10 Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making

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EP20722936.0A Active EP3856341B1 (en) 2019-04-12 2020-04-10 Crystalline forms of (s)-1-(4-fluorophenyl)-1-(2-(4-(6-(1-methyl-1h-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl)piperazinyl)-pyrimidin-5-yl)ethan-1-amine and methods of making

Country Status (20)

Country Link
US (5) US12060354B2 (https=)
EP (2) EP4302761A3 (https=)
JP (1) JP7728178B2 (https=)
CN (1) CN113966334B (https=)
CA (2) CA3296895A1 (https=)
DK (1) DK3856341T3 (https=)
ES (1) ES2966512T3 (https=)
FI (1) FI3856341T3 (https=)
HR (1) HRP20231533T1 (https=)
HU (1) HUE064283T2 (https=)
IL (2) IL287148A (https=)
LT (1) LT3856341T (https=)
MA (1) MA53759A (https=)
PL (1) PL3856341T3 (https=)
PT (1) PT3856341T (https=)
RS (1) RS64881B1 (https=)
SI (1) SI3856341T1 (https=)
SM (1) SMT202300447T1 (https=)
TW (1) TWI845657B (https=)
WO (1) WO2020210669A1 (https=)

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WO2021183709A1 (en) 2020-03-11 2021-09-16 Teva Czech Industries S.R.O Solid state forms of avapritinib and process for preparation thereof
WO2021257522A1 (en) 2020-06-17 2021-12-23 Teva Czech Industries S.R.O Solid state forms of avapritinib salts
HU231413B1 (hu) * 2021-02-26 2023-08-28 Egis Gyógyszergyár Zrt. Eljárás avapritinib és intermedierek előállítására
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HU231755B1 (hu) * 2022-08-11 2026-02-28 Egis Gyógyszergyár Zrt. Új avapritinib sók és előállítási eljárásaik
US20240382493A1 (en) * 2023-05-18 2024-11-21 Blueprint Medicines Corporation Methods for treating systemic mastocytosis and gastrointestinal stromal tumors
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US20210147433A1 (en) 2021-05-20
IL287148A (en) 2021-12-01
US11964980B2 (en) 2024-04-23
US12252494B2 (en) 2025-03-18
LT3856341T (lt) 2023-12-27
CN113966334A (zh) 2022-01-21
HRP20231533T1 (hr) 2024-03-01
EP4302761A2 (en) 2024-01-10
US20260116883A1 (en) 2026-04-30
TW202104232A (zh) 2021-02-01
PT3856341T (pt) 2023-12-12
US11999744B2 (en) 2024-06-04
IL324301A (en) 2025-12-01
US20230271971A1 (en) 2023-08-31
DK3856341T3 (da) 2023-12-04
TWI845657B (zh) 2024-06-21
SI3856341T1 (sl) 2024-02-29
ES2966512T3 (es) 2024-04-22
US12060354B2 (en) 2024-08-13
JP2022526438A (ja) 2022-05-24
CA3296895A1 (en) 2026-03-02
PL3856341T3 (pl) 2024-03-04
EP3856341B1 (en) 2023-09-06
JP7728178B2 (ja) 2025-08-22
FI3856341T3 (fi) 2023-11-30
CA3136707A1 (en) 2020-10-15
HUE064283T2 (hu) 2024-02-28
WO2020210669A1 (en) 2020-10-15
US20240132510A1 (en) 2024-04-25
RS64881B1 (sr) 2023-12-29
CN113966334B (zh) 2025-01-21
US20230124801A1 (en) 2023-04-20
EP3856341A1 (en) 2021-08-04
SMT202300447T1 (it) 2024-01-10
MA53759A (fr) 2021-08-04

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